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RU2008105590A - APPLICATION 3, 11b-CIS-DIHYDROTETRABENAZINE FOR TREATMENT OF GENTINGTON DISEASE SYMPTOMS - Google Patents

APPLICATION 3, 11b-CIS-DIHYDROTETRABENAZINE FOR TREATMENT OF GENTINGTON DISEASE SYMPTOMS Download PDF

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RU2008105590A
RU2008105590A RU2008105590/15A RU2008105590A RU2008105590A RU 2008105590 A RU2008105590 A RU 2008105590A RU 2008105590/15 A RU2008105590/15 A RU 2008105590/15A RU 2008105590 A RU2008105590 A RU 2008105590A RU 2008105590 A RU2008105590 A RU 2008105590A
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cis
dihydrotetrabenazine
patient
disease
huntington
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RU2008105590/15A
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RU2409365C2 (en
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Роберт ТРИДЖЕТТ (GB)
Роберт ТРИДЖЕТТ
Тьерри ФИЙУ (CH)
Тьерри ФИЙУ
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Кембридж Лэборетериз (Айэлэнд) Лимитед (Ie)
Кембридж Лэборетериз (Айэлэнд) Лимитед
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The invention provides 3,11b- cis -dihydrotetrabenazine for use in halting or slowing the progress of one or more symptoms of Huntington's disease in a patient, and more particularly a symptom selected from involuntary movements such as involuntary chorea, tremors and twitches, and degeneration in gait.

Claims (19)

1. 3,11b-цис-дигидротетрабеназин для применения с целью приостановки или замедления развития одного или более симптомов болезни Гентингтона у пациента, в особенности симптомов, выбранных из группы симптомов, ассоциированных с непроизвольными движениями, такими как хорея, тремор и подергивания, а также ухудшение походки.1. 3,11b-cis-dihydrotetrabenazine for use in order to suspend or slow the development of one or more symptoms of Huntington’s disease in a patient, in particular those selected from the group of symptoms associated with involuntary movements such as chorea, tremors and twitches, as well as worsening gait. 2. 3,11b-цис-дигидротетрабеназин для профилактического лечения пациента, являющегося носителем мутантной формы гена, ответственного за развитие болезни Гентингтона.2. 3,11b-cis-dihydrotetrabenazine for the prophylactic treatment of a patient carrying a mutant form of the gene responsible for the development of Huntington's disease. 3. 3,11b-цис-дигидротетрабеназин для профилактического лечения пациента в возрасте от 15 до 50 лет, являющегося носителем мутантной формы HD-гена, однако еще не развившего симптомы БГ, с целью предотвращения или замедления развития симптомов, ассоциированных с болезнью Гентингтона.3. 3,11b-cis-dihydrotetrabenazine for the prophylactic treatment of a patient aged 15 to 50 years who is a carrier of a mutant form of the HD gene, but has not yet developed symptoms of HD, in order to prevent or slow the development of symptoms associated with Huntington's disease. 4. 3,11b-цис-дигидротетрабеназин по любому из пп.1-3, где 3,11b-цис-дигидротетрабеназин находится, по существу, в чистой форме, например, препарат с изомерной чистотой более 90%, обычно более чем 95%, наиболее предпочтительно более чем 98%.4. 3,11b-cis-dihydrotetrabenazine according to any one of claims 1 to 3, where 3,11b-cis-dihydrotetrabenazine is in substantially pure form, for example, a preparation with isomeric purity of more than 90%, usually more than 95% most preferably more than 98%. 5. 3,11b-цис-дигидротетрабеназин для применения по любому из пп.1-3, где 3,11b-цис-дигидротетрабеназин находится в (+)-изомерной форме.5. 3,11b-cis-dihydrotetrabenazine for use according to any one of claims 1 to 3, wherein 3,11b-cis-dihydrotetrabenazine is in the (+) isomeric form. 6. 3,11b-цис-дигидротетрабеназин по любому пп.1-3, где соединение представляет собой соединение формулы (Iа)6. 3,11b-cis-dihydrotetrabenazine according to any one of claims 1 to 3, where the compound is a compound of formula (Ia)
Figure 00000001
Figure 00000001
 7. 3,11b-цис-дигидротетрабеназин по любому из пп.1-3 в виде кислотно-аддитивной соли.7. 3,11b-cis-dihydrotetrabenazine according to any one of claims 1 to 3 in the form of an acid addition salt. 8. 3,11b-цис-дигидротетрабеназин по п.7 в виде метансульфоната.8. 3,11b-cis-dihydrotetrabenazine according to claim 7 in the form of methanesulfonate. 9. 3,11b-цис-дигидротетрабеназин по п.5 в виде кислотно-аддитивной соли.9. 3,11b-cis-dihydrotetrabenazine according to claim 5 in the form of an acid addition salt. 10. 3,11b-цис-дигидротетрабеназин по п.9 в виде метансульфоната.10. 3,11b-cis-dihydrotetrabenazine according to claim 9 in the form of methanesulfonate. 11. Применение 3,11b-цис-дигидротетрабеназина по любому из пп.1-10 для производства лекарственного средства, предназначенного для приостановки или замедления развития одного или нескольких симптомов болезни Гентингтона у пациента, в особенности симптомов, выбранных из группы симптомов, ассоциированных с непроизвольными движениями, такими как хорея, тремор и подергивания, а также ухудшение походки.11. The use of 3,11b-cis-dihydrotetrabenazine according to any one of claims 1 to 10 for the manufacture of a medicament intended to suspend or slow down the development of one or more symptoms of Huntington's disease in a patient, especially those selected from the group of symptoms associated with involuntary movements such as chorea, tremors and twitches, as well as worsening gait. 12. Применение 3,11b-цис-дигидротетрабеназина по любому из пп.1-10 для производства лекарственного средства, предназначенного для профилактического лечения пациента, являющегося носителем мутантной формы гена, ответственного за развитие болезни Гентингтона.12. The use of 3,11b-cis-dihydrotetrabenazine according to any one of claims 1 to 10 for the manufacture of a medicament for the prophylactic treatment of a patient carrying a mutant form of the gene responsible for the development of Huntington's disease. 13. Применение 3,11b-цис-дигидротетрабеназина по любому из пп.1-10 для производства лекарственного средства, предназначенного для профилактического лечения пациента в возрасте от 15 до 50 лет, являющегося носителем мутантной формы HD-гена, однако еще не развившего симптомы БГ, с целью предотвращения или замедления развития симптомов болезни Гентингтона.13. The use of 3,11b-cis-dihydrotetrabenazine according to any one of claims 1 to 10 for the manufacture of a medicament for the prophylactic treatment of a patient aged 15 to 50 years who is a carrier of a mutant form of the HD gene, but has not yet developed symptoms of HD , in order to prevent or slow the development of symptoms of Huntington's disease. 14. Способ приостановки или замедления развития одного или нескольких симптомов болезни Гентингтона у нуждающегося в подобном лечении пациента, в особенности симптомов, выбранных из группы симптомов, ассоциированных с непроизвольными движениями, такими как хорея, тремор и подергивания, а также ухудшение походки; где способ включает введение эффективных терапевтических количеств 3,11b-цис-дигидротетрабеназина по любому из пп.1-10.14. A method of suspending or slowing down the development of one or more symptoms of Huntington's disease in a patient in need of such treatment, especially those selected from the group of symptoms associated with involuntary movements, such as chorea, tremors and twitches, as well as worsening of the gait; where the method includes the introduction of effective therapeutic amounts of 3,11b-cis-dihydrotetrabenazine according to any one of claims 1 to 10. 15. Способ профилактического лечения пациента, являющегося носителем мутантной формы гена, ответственного за развитие болезни Гентингтона, включающий введение цис-дигидротетрабеназина по любому из пп.1-10 в количествах, эффективных для предотвращения или замедления развития симптомов болезни Гентингтона.15. A method for the prophylactic treatment of a patient carrying a mutant form of the gene responsible for the development of Huntington's disease, comprising administering the cis-dihydrotetrabenazine according to any one of claims 1 to 10 in amounts effective to prevent or slow the development of symptoms of Huntington's disease. 16. Соединение по п.2, где пациент, которому вводится 3,11b-цис-дигидротетрабеназин, является носителем мутантной формы гена IT-15, в которой число CAG-повторов составляет по меньшей мере 35, обычно по меньшей мере 40, например, по меньшей мере 45 или по меньшей мере 50.16. The compound according to claim 2, where the patient, which is administered 3,11b-cis-dihydrotetrabenazine, is a carrier of the mutant form of the IT-15 gene, in which the number of CAG repeats is at least 35, usually at least 40, for example, at least 45 or at least 50. 17. Применение по п.12, где пациент, которому вводится 3,11b-цис-дигидротетрабеназин, является носителем мутантной формы гена IT-15, в которой число CAG-повторов составляет по меньшей мере 35, обычно по меньшей мере 40, например, по меньшей мере 45 или по меньшей мере 50.17. The use of claim 12, wherein the patient to whom 3,11b-cis-dihydrotetrabenazine is administered is a carrier of a mutant form of the IT-15 gene, in which the number of CAG repeats is at least 35, usually at least 40, for example at least 45 or at least 50. 18. Способ по п.15, где пациент, которому вводится 3,11b-цис-дигидротетрабеназин, является носителем мутантной формы гена IT-15, в которой число CAG-повторов составляет по меньшей мере 35, обычно по меньшей мере 40, например по меньшей мере 45 или по меньшей мере 50.18. The method according to clause 15, where the patient who is administered 3,11b-cis-dihydrotetrabenazine, is a carrier of a mutant form of the gene IT-15, in which the number of CAG repeats is at least 35, usually at least 40, for example at least 45 or at least 50. 19. Способ профилактического лечения пациента, являющегося носителем мутантной формы гена, ответственного за развитие болезни Гентингтона, включающий введение пациенту цис-дигидротетрабеназина по любому из пп.1-10 в количествах, эффективных для предотвращения или замедления субклинической прогрессии болезни Гентингтона. 19. A method for the prophylactic treatment of a patient carrying a mutant form of the gene responsible for the development of Huntington's disease, comprising administering to the patient cis-dihydrotetrabenazine according to any one of claims 1 to 10 in amounts effective to prevent or slow down the subclinical progression of Huntington's disease.
RU2008105590/15A 2005-07-14 2006-07-13 APPLICATION OF 3,11b-CIS-DIHYDROTETRABENAZINE FOR TREATMENT OF HUNTINGTON'S DISORDER SYMPTOMS RU2409365C2 (en)

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GBGB0514501.6A GB0514501D0 (en) 2005-07-14 2005-07-14 Pharmaceutical compounds
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US (1) US20080319000A1 (en)
EP (2) EP2027861B1 (en)
JP (1) JP2009501202A (en)
KR (1) KR20080030666A (en)
CN (1) CN101282726A (en)
AT (2) ATE522215T1 (en)
AU (1) AU2006268098B2 (en)
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CY (1) CY1108653T1 (en)
DE (1) DE602006002982D1 (en)
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GB (1) GB0514501D0 (en)
HR (1) HRP20080677T3 (en)
ME (1) ME01629B (en)
NZ (1) NZ565522A (en)
PL (1) PL1885363T3 (en)
PT (1) PT1885363E (en)
RS (1) RS50626B (en)
RU (1) RU2409365C2 (en)
SI (1) SI1885363T1 (en)
WO (1) WO2007007105A1 (en)
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